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1. 发明申请

WO2007019180A3 COMPOUNDS FOR BINDING TO ERALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF 审中-公开
标题翻译：用于结合至ERALPHA / BETA和GPR30的化合物，通过这些受体介导的治疗疾病状态和条件的方法及其鉴定
公开(公告)号：WO2007019180A3
公开(公告)日：2008-04-10
申请号：PCT/US2006030130
申请日：2006-08-02
申请人： STC UNM , CHEMDIV INC , ARROWHEAD CT INC , PROSSNITZ ERIC R , TKATCHENKO SERGEY E , REVANKAR CHETANA M , SKLAR LARRY A , ARTERBURN JEFFREY B , CIMINO DANIEL F , OPREA TUDOR I , BOLOGA CRISTIAN-GEORGE , EDWARDS BRUCE S , KISELYOV ALEXANDOR , YOUNG SUSAN M
发明人： PROSSNITZ ERIC R , TKATCHENKO SERGEY E , REVANKAR CHETANA M , SKLAR LARRY A , ARTERBURN JEFFREY B , CIMINO DANIEL F , OPREA TUDOR I , BOLOGA CRISTIAN-GEORGE , EDWARDS BRUCE S , KISELYOV ALEXANDOR , YOUNG SUSAN M
IPC分类号： A61K31/435 , C07D215/04 , C07D215/12 , C07D215/16 , C07D221/06 , C07D405/10 , C07D491/048 , C07D491/052 , C07D491/147
CPC分类号： C07D221/16 , C07D405/04 , C07D405/14
摘要： The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ERa and ERß). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.
摘要翻译：本发明在分子生物学/药理学领域，并提供调节GPR30以及经典雌激素受体α和β（ERα和ERβ）的作用的化合物。这些化合物可以用作一种或多种所公开的雌激素受体的激动剂和/或拮抗剂。通过这些受体中的一种或多种介导的疾病包括癌症（特别是乳腺，生殖和其他激素依赖性癌症，白血病，结肠癌，前列腺癌），生殖（泌尿 - 泌尿）包括子宫内膜炎，前列腺炎，多囊卵巢综合征，膀胱控制，激素相关疾病，听觉障碍，心血管疾病，包括潮热和大量出汗，高血压，中风，肥胖，骨质疏松症，血液病，血管疾病或诸如静脉血栓形成，动脉粥样硬化等疾病，以及许多其他疾病和中枢和周围神经系统，包括抑郁症，失眠，焦虑，多发性硬化，神经病变，神经变性疾病如帕金森病和阿尔茨海默病，以及炎性肠病，克罗恩病，腹腔（腹腔）疾病和肠道相关疾病。用于预防或减少性交后怀孕的可能性的避孕指示是本发明的另一方面。

2. 发明申请

WO2009070331A3 COMPOUNDS AND METHODS FOR THE SELECTIVE INHIBITION OF ABCB1, ABCC1 AND ABCG2 TRANSPORTERS AND THE TREATMENT OF CANCERS, ESPECIALLY DRUG RESISTANT CANCERS AND HIGH THROUGHPUT FLOW CYTOMETRY ASSAY TO DETECT SELECTIVE INHIBITORS 审中-公开
标题翻译：选择性抑制ABCB1，ABCC1和ABCG2转运蛋白以及治疗癌症，特别是抗药性癌症和高通量流式细胞测定以检测选择性抑制剂的化合物和方法
公开(公告)号：WO2009070331A3
公开(公告)日：2009-07-23
申请号：PCT/US2008013209
申请日：2008-11-28
申请人： STC UNM , LARSON RICHARD S , SKLAR LARRY A , EDWARDS BRUCE S , IVNITSKI-STEELE IRENA D , OPREA TUDOR I , LOVATO DEBBIE M , KHAWAJA HADYA M , WINTER STUART S , YOUNG SUSAN M
发明人： SKLAR LARRY A , EDWARDS BRUCE S , IVNITSKI-STEELE IRENA D , OPREA TUDOR I , LOVATO DEBBIE M , KHAWAJA HADYA M , WINTER STUART S , YOUNG SUSAN M
IPC分类号： A61K31/415 , A61K31/12 , A61P35/00
CPC分类号： A61K31/12 , A61K31/415 , A61K45/06 , A61K2300/00
摘要： Compounds disclosed which inhibit ABCBl transporter protein are useful for treating diseases in which ABCBl transporter protein mediates the disease state, including numerous cancers, including hematopoietic cancers, including various leukemias, especially T-lineage acute lymphoblastic leukemia, as well as cancerous tumors, especially forms which exhibit multiple drug resistance. Pharmaceutical compositions which comprise an inhibitor of ABCBl transporter protein and at least one additional anticancer agent, optionally in combination with a pharmaceutically acceptable carrier, additive or excipient are another aspect of the present invention. A flow cytometry based, high-throughput screening (HST) assay that quantifies ABCBl efflux is also disclosed. Methods of identifying inhibitors of ABCBl, ABCG2 and ABCCl transporter proteins are also disclosed.
摘要翻译：公开的抑制ABCB1转运蛋白的化合物可用于治疗其中ABCB1转运蛋白介导疾病状态的疾病，包括多种癌症，包括造血系统癌症，包括各种白血病，尤其是T-系急性淋巴细胞白血病，以及癌性肿瘤，特别是癌表现出多重耐药性。包含ABCB1转运蛋白抑制剂和至少一种另外的抗癌剂，任选地与药学上可接受的载体，添加剂或赋形剂组合的药物组合物是本发明的另一方面。还公开了量化ABCB1流出的基于流式细胞术的高通量筛选（HST）测定法。还公开了鉴定ABCB1，ABCG2和ABCCl转运蛋白的抑制剂的方法。

3. 发明申请

WO2009148623A3 METHODS AND RELATED COMPOSITIONS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的方法和相关组合物
公开(公告)号：WO2009148623A3
公开(公告)日：2010-03-25
申请号：PCT/US2009003438
申请日：2009-06-05
申请人： STC UNM , THOMPSON TODD A , MACKENZIE DEBRA , OPREA TUDOR I , SKLAR LARRY A , EDWARDS BRUCE S , HAYNES MARK
发明人： THOMPSON TODD A , MACKENZIE DEBRA , OPREA TUDOR I , SKLAR LARRY A , EDWARDS BRUCE S , HAYNES MARK
IPC分类号： A61K31/445 , A61K31/165 , A61P35/00
CPC分类号： A61K31/437 , A61K31/135 , A61K31/165 , A61K31/445 , A61K45/06 , A61N5/10
摘要： A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death. While the exact mechanism of cancer cell degradation and death is not completely understood, the treated cancer cells, including refractory prostate cancer cells, give indications of cell death through an autophagic mechanism. Pharmaceutical compositions related to the presently disclosed methods are also disclosed.
摘要翻译：治疗和/或预防癌症的方法包括在癌细胞中引起增加的细胞内颗粒度的给药剂，至少足以抑制这种细胞增殖的量，优选以足以导致癌细胞死亡的量。该方法特别涉及难治性癌症，特别是激素难治性前列腺癌。所鉴定的试剂导致癌细胞中细胞内的粒度增加，并将粘附的癌细胞转化为非粘附的癌细胞，导致癌细胞死亡。使用本发明，癌细胞在相对低的药物浓度下经历增加的细胞内粒度，同时也抑制细胞增殖。增加的浓度导致粘附的癌细胞转化为非粘附的癌细胞，然后转移到细胞死亡。虽然癌细胞降解和死亡的确切机制尚未完全了解，但治疗的癌细胞（包括难治性前列腺癌细胞）通过自噬机制给予细胞死亡的指示。还公开了与目前公开的方法相关的药物组合物。

4. 发明申请

WO2011094260A3 NOVEL BIFUNCTIONAL METNASE/INTNASE INHIBITORS AND RELATED COMPOSITIONS AND METHODS OF TREATMENT OF CANCER 审中-公开
标题翻译：新型双功能蛋白酶/终止抑制剂及相关组合物及治疗癌症的方法
公开(公告)号：WO2011094260A3
公开(公告)日：2011-12-01
申请号：PCT/US2011022508
申请日：2011-01-26
申请人： STC UNM , HROMAS ROBERT , LEITAO ANDREI , OPREA TUDOR I , SKLAR LARRY A , WILLIAMSON ELIZABETH A , WRAY JUSTIN , WANG WEI
发明人： HROMAS ROBERT , LEITAO ANDREI , OPREA TUDOR I , SKLAR LARRY A , WILLIAMSON ELIZABETH A , WRAY JUSTIN , WANG WEI
IPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61P35/00 , C07D401/04 , C07D401/14
CPC分类号： C07D215/56 , A61K31/47 , A61K31/4709 , A61K31/475 , A61K31/496 , A61K31/7048 , A61K45/06 , A61N5/1001 , A61N5/1045 , A61N2005/1087 , A61N2005/1098 , C07D401/06 , C07D401/10 , C07D401/12 , A61K2300/00
摘要： This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-I) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers. In certain aspects of such treatments, compounds, compositions and methods of treatment of the invention are administered as a monotherapy (in some cases, to patients who have exhibited resistance to Topo IIalpha inhibitors such as VP- 16), or are co-administered with a Topo IIalpha inhibitor or other anti-cancer agents as otherwise described herein or in combination with radiation therapy.
摘要翻译：本发明涉及新的癌症治疗组合物和相关的治疗方法。更具体地说，本发明部分涉及同时损伤DNA的DNA复制和修复蛋白质Metnase和/或Intnase（也称为Gypsy整合酶，Gypsy Integrease-1，Gypsy Retransposon Integrase 1或GIN-1）的小型化学双功能抑制剂，以及利用抑制剂增加包括放射治疗在内的癌症治疗方案的有效性的治疗方法。在优选的实施方案中，本发明的化合物，组合物和治疗方法用于治疗患有白血病的患者（例如急性骨髓性白血病（AML）和相关的癌症）。在这些治疗的某些方面，化合物，组合物和治疗方法本发明作为单一疗法（在某些情况下，对已显示出对Topo IIalpha抑制剂如VP-16具有抗性的患者）施用，或者与本文另有描述的Topo IIal抑制剂或其它抗癌剂共同施用，或结合放射治疗。

5. 发明申请

WO2010114919A2 METNASE AND INTNASE INHIBITORS AND THEIR USE IN TREATING CANCER 审中-公开
标题翻译： METNASE和INTNASE抑制剂及其在治疗癌症中的应用
公开(公告)号：WO2010114919A2
公开(公告)日：2010-10-07
申请号：PCT/US2010029462
申请日：2010-03-31
申请人： STC UNM , HROMAS ROBERT , LEITAO ANDREI , OPREA TUDOR I , SKLAR LARRY A , WILLIAMSON ELIZABETH A , WRAY JUSTIN
发明人： HROMAS ROBERT , LEITAO ANDREI , OPREA TUDOR I , SKLAR LARRY A , WILLIAMSON ELIZABETH A , WRAY JUSTIN
IPC分类号： A61K31/4365 , A61K31/38 , A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/47 , A61P35/00
CPC分类号： A61K31/38 , A61K31/4353 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/47
摘要： This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical inhibitors of DNA repair proteins (Metnase) and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols.
摘要翻译：本发明涉及新的癌症治疗组合物和相关的治疗方法。更具体地，本发明部分涉及DNA修复蛋白（Metnase）的小化学抑制剂以及利用抑制剂增加癌症治疗方案的有效性的治疗方法。

6. 发明专利

AU2003302462A8 Bead-based detection of ligand-gpcr-g protein complexes 未知
公开(公告)号：AU2003302462A8
公开(公告)日：2004-06-18
申请号：AU2003302462
申请日：2003-05-05
申请人： PROSSNITZ ERIC R , KEY ALEX T , SHI MEI , BURANDA TIONE , SKLAR LARRY A , NEUBIG RICHARD , SIMONS PETER C , CIMINO DANIEL , SCIENCE AND TECHNOLOGY CORP UN
发明人： KEY ALEX T , BURANDA TIONE , CIMINO DANIEL , SKLAR LARRY A , PROSSNITZ ERIC R , NEUBIG RICHARD , SHI MEI , SIMONS PETER C
IPC分类号： B01F13/00 , B01F15/02 , C07D233/76 , C07D401/12 , C07D405/12 , C12N5/02 , C12P21/04 , C12Q1/00 , C12P27/00 , C07K17/00 , C07K7/00 , G01N33/53 , C12Q1/68
摘要： The present invention provides a compound and a method of making a compound according to the following formula: where R 1 is an alkyl group having 1 to 12 carbons; R 2 is a urea group; R 3 is an active group, such as fluorescein, a toxin, radiolabel or drug; and R 4 , R 5 and R 6 are each independently a halide group.

7. 发明专利

AU2003302462A1 BEAD-BASED DETECTION OF LIGAND-GPCR-G PROTEIN COMPLEXES 未知
公开(公告)号：AU2003302462A1
公开(公告)日：2004-06-18
申请号：AU2003302462
申请日：2003-05-05
申请人： CIMINO DANIEL , BURANDA TIONE , KEY ALEX T , NEUBIG RICHARD , SCIENCE AND TECHNOLOGY CORP UN , SKLAR LARRY A , PROSSNITZ ERIC R , SIMONS PETER C , SHI MEI
发明人： BURANDA TIONE , KEY ALEX T , NEUBIG RICHARD , SKLAR LARRY A , PROSSNITZ ERIC R , SIMONS PETER C , SHI MEI , CIMINO DANIEL
IPC分类号： B01F13/00 , B01F15/02 , C07D233/76 , C07D401/12 , C07D405/12 , C12N5/02 , C12P21/04
摘要： The present invention provides a compound and a method of making a compound according to the following formula: where R 1 is an alkyl group having 1 to 12 carbons; R 2 is a urea group; R 3 is an active group, such as fluorescein, a toxin, radiolabel or drug; and R 4 , R 5 and R 6 are each independently a halide group.

8. 发明申请

WO2004048922A2 BEAD-BASED DETECTION OF LIGAND-GPCR-G PROTEIN COMPLEXES 审中-公开
标题翻译：基于珠粒检测的LIGAND-GPCR-G蛋白复合物
公开(公告)号：WO2004048922A2
公开(公告)日：2004-06-10
申请号：PCT/US0313851
申请日：2003-05-05
申请人： SCIENCE AND TECHNOLOGY CORP UN , SKLAR LARRY A , PROSSNITZ ERIC R , SIMONS PETER C , SHI MEI , CIMINO DANIEL , BURANDA TIONE , KEY ALEX T , NEUBIG RICHARD
发明人： SKLAR LARRY A , PROSSNITZ ERIC R , SIMONS PETER C , SHI MEI , CIMINO DANIEL , BURANDA TIONE , KEY ALEX T , NEUBIG RICHARD
IPC分类号： B01F13/00 , B01F15/02 , C07D233/76 , C07D401/12 , C07D405/12 , C12N5/02 , C12P21/04 , G01N
CPC分类号： C07D401/12 , B01F13/0059 , B01F13/0093 , B01F13/0096 , B01F15/0201 , B01F15/024 , C07D233/76 , C07D405/12
摘要： The present invention provides a general approach for G protein coupled receptors that may be used to define agonists and antagonists, and the specificity of receptor coupling to G protein subunits. Methods of the present invention use small volumes (microliters) and are compatible with high throughput flow cytometry. When assays of the present invention are multiplexed, the specificity of the interactions of a receptor with many G proteins may be determined simultaneously.
摘要翻译：本发明提供了可用于定义激动剂和拮抗剂的G蛋白偶联受体的一般方法以及受体与G蛋白亚基偶联的特异性。本发明的方法使用小体积（微升）并且与高通量流式细胞术兼容。当本发明的测定被复用时，可以同时测定受体与许多G蛋白的相互作用的特异性。

9. 发明申请

WO2011119732A2 METHOD FOR INTEGRIN LIGAND DISCOVERY 审中-公开
标题翻译：集成配对发现方法
公开(公告)号：WO2011119732A2
公开(公告)日：2011-09-29
申请号：PCT/US2011029627
申请日：2011-03-23
申请人： STC UNM , CHIGAEV ALEXANDRE , SKLAR LARRY A
发明人： CHIGAEV ALEXANDRE , SKLAR LARRY A
IPC分类号： G01N33/53 , A61K31/42 , C07D261/08 , G01N33/15 , G01N33/533 , G01N33/577
CPC分类号： G01N33/5041 , A61K31/195 , A61K31/197 , A61K31/357 , A61K31/36 , A61K31/42 , G01N33/5055 , G01N33/68 , G01N2333/70546 , G01N2333/7055 , G01N2500/04 , G01N2500/10
摘要： This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery base upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.
摘要翻译：本发明一般涉及整合素配体发现和基于诱导配体诱导表位的整联蛋白配体发现的方法。这样的配体具有作为抗炎，抗血管生成和/或抗血栓形成剂的活性剂的潜力，并且用于治疗整联蛋白介导的疾病和/或病症。

10. 发明申请

WO2012154975A3 NITRIC OXIDE/CGMP PATHWAY INHIBITION OF VLA-4 RELATED CELL ADHESION 审中-公开
标题翻译：硝酸氧化酶/ CGMP途径抑制VLA-4相关细胞粘附
公开(公告)号：WO2012154975A3
公开(公告)日：2013-03-21
申请号：PCT/US2012037352
申请日：2012-05-10
申请人： STC UNM , CHIGAEV ALEXANDRE , SKLAR LARRY A
发明人： CHIGAEV ALEXANDRE , SKLAR LARRY A
IPC分类号： A61K31/4162 , A61K31/34 , A61K31/506 , A61K31/519 , A61K31/52 , A61P35/00
CPC分类号： A61K31/708 , A61K31/132 , A61K31/506 , A61K31/655 , A61K31/665 , A61K45/06 , G01N33/5008 , G01N33/57488 , G01N2500/10 , G01N2800/50
摘要： The invention provides methods of treating nitric oxide/cGMP pathway-cell adhesion disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention relates to a method for down-regulating alpha4beta1-integrin affinity and inhibiting and reversing adhesion formation in patients or subjects in need using a nitric oxide donor.
摘要翻译：本发明提供了治疗一氧化氮/ cGMP途径 - 细胞粘附病症和相关药物组合物，诊断，筛选技术和试剂盒的方法。在一个实施方案中，本发明涉及一种用于下调α4β1整联蛋白亲和力并抑制和逆转使用一氧化氮供体的患者或需要受试者的粘连形成的方法。

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